US2007154396A1PendingUtilityA1

Block copolymers and nano micelles comprising the same

Assignee: IND TECH RES INSTPriority: Dec 30, 2005Filed: Jun 7, 2006Published: Jul 5, 2007
Est. expiryDec 30, 2025(expired)· nominal 20-yr term from priority
A61K 47/6907A61K 49/1806A61K 49/126A61K 47/593A61K 47/59A61K 47/551
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Claims

Abstract

A block copolymer. The block copolymer has formula A-B-C, wherein A represents polyester, B represents polyamide, and C represents specific molecular groups or metal complexes. The invention also provides a nano micelle and drug carrier including the block copolymer.

Claims

exact text as granted — not AI-modified
1 . A block copolymer having formula A-B-C, wherein A comprises polyester, B comprises polyamide, and C comprises specific molecular groups or metal complexes. 
     
     
         2 . The block copolymer as claimed in  claim 1 , wherein the block copolymer comprises diblock copolymer. 
     
     
         3 . The block copolymer as claimed in  claim 1 , wherein the polyester comprises polylactide (PLA) or derivatives thereof. 
     
     
         4 . The block copolymer as claimed in  claim 1 , wherein the polyamide comprises polyoxazoline (POz) or derivatives thereof. 
     
     
         5 . The block copolymer as claimed in  claim 1 , wherein the specific molecular group recognizes cancer cells. 
     
     
         6 . The block copolymer as claimed in  claim 1 , wherein the specific molecular group comprises folate. 
     
     
         7 . The block copolymer as claimed in  claim 6 , wherein the block copolymer has formula (I) 
       
         
           
           
               
               
           
         
         wherein L comprises hydrogen or C1-6 alkyl, Z comprises hydrogen, C2-21 acyl, or C2-21 benzyl, Q comprises initiators for ring-opening polymerization, G comprises acyl or ester groups, and x and y are 1˜10,000. 
       
     
     
         8 . The block copolymer as claimed in  claim 7 , wherein the initiator for ring-opening polymerization comprises hydrogen, alkyl, or hydroxyl groups. 
     
     
         9 . The block copolymer as claimed in  claim 7 , wherein y/x is 0.1˜1,000. 
     
     
         10 . The block copolymer as claimed in  claim 1 , wherein the specific molecular group comprises antibody. 
     
     
         11 . The block copolymer as claimed in  claim 1 , wherein the metal complex comprises magnetic resonance imaging (MRI) contrast agents. 
     
     
         12 . The block copolymer as claimed in  claim 11 , wherein the MRI contrast agent comprises chelates formed by diethylenetriaminepentaacetic acid (DTPA) and gadolinium ions (Gd 3+ ) or indium ( 111 In). 
     
     
         13 . The block copolymer as claimed in  claim 12 , wherein the chelate formed by diethylenetriaminepentaacetic acid (DTPA) and gadolinium ions (Gd 3+ ) or indium ( 111 In) has a chelating ratio of about 1˜100 wt %. 
     
     
         14 . The block copolymer as claimed in  claim 12 , wherein the block copolymer has formula (II) 
       
         
           
           
               
               
           
         
         wherein D comprises hydrogen or C1-6 alkyl, E comprises hydrogen, C2-21 acyl, or C2-21 benzyl, Q comprises initiators for ring-opening polymerization, G comprises acyl or ester groups, and a and b are 1˜10,000. 
       
     
     
         15 . The block copolymer as claimed in  claim 14 , wherein the initiator for ring-opening polymerization comprises hydrogen, alkyl, or hydroxyl groups. 
     
     
         16 . The block copolymer as claimed in  claim 14 , wherein b/a is 0.1˜1,000. 
     
     
         17 . A nano micelle comprising a plurality of block copolymers as claimed in  claim 1  or a plurality of block copolymers comprising specific molecular groups and metal complexes. 
     
     
         18 . The nano micelle as claimed in  claim 17 , wherein the nano micelle has a hydrophobic interior and hydrophilic exterior. 
     
     
         19 . The nano micelle as claimed in  claim 17 , wherein the nano micelle has a diameter of about 10˜1,000 nm. 
     
     
         20 . The nano micelle as claimed in  claim 17 , wherein the nano micelle has a diameter of about 20˜200 nm. 
     
     
         21 . The nano micelle as claimed in  claim 17 , wherein the nano micelle has critical micelle concentration (CMC) of about 0.0001˜1 mg/mL. 
     
     
         22 . The nano micelle as claimed in  claim 17 , wherein the nano micelle has a relaxivity of about 5.0˜6.0(mM·s) − . 
     
     
         23 . A nano drug carrier, comprising:
 a nano micelle as claimed in  claim 17 ; and   a drug encapsulated thereinto.   
     
     
         24 . The nano drug carrier as claimed in  claim 23 , wherein the drug comprises water-insoluble drugs. 
     
     
         25 . The nano drug carrier as claimed in  claim 23 , wherein the drug comprises camptothecin, doxorubicin, or derivatives thereof. 
     
     
         26 . The nano drug carrier as claimed in  claim 23 , wherein the nano drug carrier is delivered by oral, transdermal administration, injection, or inhalation.

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